神經(jīng)系統(tǒng)藥理-魏爾清抗癲癇藥課件

1、Psychomotor seizuresPetit mal (absence)Grand mal (tonic-clonic)Epilepsy is not a single entity; it is a family of different recurrent seizure disorders that have in common the sudden, excessive and disorderly discharge of central neurons. This results in abnormal movement or perceptions that are of

2、short duration but that tend to recur.Psychomotor seizuresPetit mal Classification of epilepsy (older)Generalized seizures (全身發(fā)作）Grand mal（大發(fā)作）： tonic-clonic seizures（強(qiáng)直陣攣）Petit mal （小發(fā)作） ： absence seizures （失神發(fā)作）Partial seizures (部分性發(fā)作)Pshychomotor（精神運(yùn)動(dòng)性）： temporal lobe seizures（顳葉癲癇）Partial（部分發(fā)作）：

3、 motor, sensory, ANS, etc.（局限性發(fā)作）Classification of epilepsy (olClassification of epilepsyClassification of epilepsyNormal EEGAbsence EEGNormal EEGAbsence EEGThe pathways for seizure propagation in partial seizures and primary generalized seizuresThe pathways for seizure propa神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件Stereotyp

4、ical complex partial seizuresStereotypical complex partial Ineffective for petit mal (absence seizures)(3) AntiarrhythmiaNecessary to monitor plasma concentrations(1) Grand mal / Partial：Broad spectrum of antiepilepsyIneffective for petit mal (absence seizures)Phenytoin, Carbamazepine, Phenobarbital

5、Adverse effects：Antiepileptic drugsHepatic toxicityGrand mal, status epilepticus;Mephenytoin 美芬妥英, Ethotoin 乙苯妥英： analogues of phenytoinInduction of hepatic drug-metabolizing enzymes(3) Antiarrhythmia(3) AntiarrhythmiaAntiepileptic drugsPsychomotor seizuresLamotrigine 拉莫三嗪Primidone, Valproate sodium

6、Principals of antiepileptic drug usesMechanisms of antiepileptic drugsElectrophysiologicalInhibiting excessive dischargesInhibiting spread of dischargesMolecularPotentiating GABA neuronal functionsModulating Na+, Ca2+, K+channel fuctionsIneffective for petit mal (absA. Antiepileptic drugsSpecial dru

7、gsPhenytoin Sodium 苯妥英鈉A. Antiepileptic drugsSpecial1. Pharmacological effects and the mechanism Inhibiting influx of Na+ and Ca2+ Inhibiting spread of abnormal dischargesA. Antiepileptic drugs1. Pharmacological effects and神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件2. Clinical uses(1) AntiepilepsyGrand mal, status epilepticus;

8、 Partial seizures (simple and complex);Ineffective for petit mal (absence seizures)(2) Trigeminal and related neuralgia(3) AntiarrhythmiaA. Antiepileptic drugs2. Clinical usesA. Antiepilep3. ADME Larger doses: non-linear kinetics（plasma concentration 10 g/ml）Necessary to monitor plasma concentration

9、s Induction of hepatic drug-metabolizing enzymesA. Antiepileptic drugsA. Antiepileptic drugs神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件3. Adverse effects(1) Local reactionsGI reactions; gingival hyperplasia(2) CNS reactionsParticularly in the cerebellum and vestibular systems: nystagmus (眼球震顫), ataxia (共濟(jì)失調(diào)), et

10、c.Behavioral changes: confusion, hallucination A. Antiepileptic drugs3. Adverse effectsA. Antiepil(3) Hemological reactionsMegaloblastic anemia(4) Allergic reactionsSkin reactions; blood cell abnormality (including thrombocytopenia, agranulocytosis);hepatic toxicity; ect.(5) Skeletal reactionsOsteom

11、alacia by abnormal vitamin D metabolism and calcium absorptionA. Antiepileptic drugs(3) Hemological reactionsA. A4. Drug interactions(1) Increases plasma concentrations of drugs by displacement of plasma protein binding (salicylates) and inhibition of inactivation (isoniazid, chloramphenicol)(2) Dec

12、reases plasma concentrations of drugs (phenobarbital, carbamazepine) by enhancing metabolism(3) Phenytoin enhances the metabolism of corticosteroids and vitamin DA. Antiepileptic drugs4. Drug interactionsA. AntiepEffective for psychomotor seizures, and grand malEpilepsy is not a single entity; it is

13、 a family of different recurrent seizure disorders that have in common the sudden, excessive and disorderly discharge of central neurons.(2) Trigeminal and related neuralgiaPhenytoin, Carbamazepine, PhenobarbitalThis results in abnormal movement or perceptions that are of short duration but that ten

14、d to recur.Other anticovulsant drugsParticularly in the cerebellum and vestibular systems: nystagmus (眼球震顫), ataxia (共濟(jì)失調(diào)), etc.Adverse effectsPartial（部分發(fā)作）：Primidone, Valproate sodiumDrug interactionsPartial seizures (simple and complex);Phenytoin, Carbamazepine, PhenobarbitalInhibiting spread of d

15、ischargesCHCOOHPrincipals of antiepileptic drug usesPetit mal （小發(fā)作） ：Classification of epilepsyPrincipals of antiepileptic drug usesvasodilatation, BP ;(1) AntiepilepsyInhibiting both formation and spread of dischargesEffective for grand mal, partial simple seizures, status epilepticusPhenobarbital

16、苯巴比妥A. Antiepileptic drugsEffective for psychomotor seizEffective for psychomotor seizures, and grand malEffective for mania, depression, and neuralgiaCarbamazepine 卡馬西平A. Antiepileptic drugsEffective for psychomotor seiz神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件Broad spectrum of antiepilepsyHepatic toxicityValproate sodium 丙

17、戊酸鈉A. Antiepileptic drugsCH3CH2CH2 CHCOOHCH3CH2CH2Valproate sodium 丙戊酸鈉A. AntOther antiepileptic drugsPrimidone 撲米酮：analogues of phenobarbital, used for phenobarbital- and phenytoin-ineffective patientsMephenytoin 美芬妥英, Ethotoin 乙苯妥英： analogues of phenytoinEthosuximide 乙琥胺：peptit malDiazepam: status

18、 epilepticus (i.v.)Nitrozepam 硝西泮, Clonazepam 氯硝西泮：peptit malLamotrigine 拉莫三嗪A. Antiepileptic drugsOther antiepileptic drugsA. A神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件Box Common toxicity of antiepileptic drugs: CNS reactions Hemological reactions Hepatic toxicityA. Antiepileptic

19、 drugsBox Common toxicity of A. An(1) AntiepilepsyPrimidone, Valproate sodiumplasma concentration monitoring if necessaryClassification of epilepsy (older)CHCOOHParticularly in the cerebellum and vestibular systems: nystagmus (眼球震顫), ataxia (共濟(jì)失調(diào)), etc.Antiepileptic drugsInduction of hepatic drug-me

20、tabolizing enzymes), Phenobrbital (i.Effective for psychomotor seizures, and grand malClassification of epilepsy (older)Partial seizures (simple and complex);Other anticovulsant drugs(2) Peptit mal: Ethosuximide(2) CNS reactions(3) Phenytoin enhances the metabolism of corticosteroids and vitamin DCh

21、oice of drugs(1) Increases plasma concentrations of drugs by displacement of plasma protein binding (salicylates) and inhibition of inactivation (isoniazid, chloramphenicol)hypertension crisis), Phenobrbital (i.Mechanisms of antiepileptic drugsvasodilatation, BP ;small larger doses;hypertension cris

22、istonic-clonic seizures（強(qiáng)直陣攣）Primidone, Valproate sodiumClinical uses(2) Peptit mal: Ethosuximiderelaxing skeletal musclesCHCOOHInhibiting both formation and spread of dischargesCHCOOHStereotypical complex partial seizures(2) CNS reactionsSpecial drugsAntiepileptic drugsNecessary to monitor plasma c

23、oncentrationsOther anticovulsant drugsMechanisms of antiepileptic drugsIneffective for petit mal (absence seizures)temporal lobe seizures（顳葉癲癇）dose individualization;Principals of antiepileptic drug uses1. Choice of drugs(1) Grand mal / Partial： Phenytoin, Carbamazepine, Phenobarbital Primidone, Val

24、proate sodium(2) Peptit mal: Ethosuximide Clonazepam, Valproate sodium(3) Psychomotor：Carbamazepine, Phenytoin(4) Status epilepticus：Diazepan (i.v.) Phenytoin (i.v.), Phenobrbital (i.m.)A. Antiepileptic drugs(1) Antiepilepsyvasodilatation2. Dosage： small larger doses; dose individualization; plasma

25、concentration monitoring if necessary3. Usage： drug combination4. Withdrawal：gradually and slowlyA. Antiepileptic drugs2. Dosage：A. Antiepileptic dr1. Effects：central depression; vasodilatation, BP ; relaxing skeletal muscles2. Uses：convulsion；hypertension crisis3. Adverse effects：depression of resp

26、iratory and vasomotor centers, antagonized by calcium preparations (i.v.)Magnesium Sulfate 硫酸鎂A. Anticonvulsant drugs1. Effects：central depression;Other anticovulsant drugsSedative-hypnotic drugsA. Anticonvulsant drugsOther anticovulsant drugsA. AMechanisms of antiepileptic drugsElectrophysiological

27、Inhibiting excessive dischargesInhibiting spread of dischargesMolecularPotentiating GABA neuronal functionsModulating Na+, Ca2+, K+channel fuctionsMechanisms of antiepileptic dr2. Clinical uses(1) AntiepilepsyGrand mal, status epilepticus; Partial seizures (simple and complex);Ineffective for petit

28、mal (absence seizures)(2) Trigeminal and related neuralgia(3) AntiarrhythmiaA. Antiepileptic drugs2. Clinical usesA. Antiepilep神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件Broad spectrum of antiepilepsyHepatic toxicityValproate sodium 丙戊酸鈉A. Antiepileptic drugsCH3CH2CH2 CHCOOHCH3CH2CH2Valproate sodium 丙戊酸鈉A. Ant神經(jīng)系統(tǒng)藥理魏爾清抗癲癇藥課件to

29、nic-clonic seizures（強(qiáng)直陣攣）Primidone, Valproate sodiumPsychomotor seizuresPrincipals of antiepileptic drug usesInhibiting influx of Na+ and Ca2+Induction of hepatic drug-metabolizing enzymes(1) Grand mal / Partial：This results in abnormal movement or perceptions that are of short duration but that ten

30、d to recur.Potentiating GABA neuronal functions), Phenobrbital (i.Partial seizures (simple and complex);Antiepileptic drugsChoice of drugsEthosuximide 乙琥胺：peptit mal(1) Grand mal / Partial：depression of respiratory and vasomotor centers, antagonized by calcium preparations (i.Mephenytoin 美芬妥英, Ethot

31、oin 乙苯妥英： analogues of phenytoinMechanisms of antiepileptic drugsPhenytoin, Carbamazepine, PhenobarbitalClassification of epilepsy (older)Classification of epilepsy (older)(3) AntiarrhythmiaCHCOOHGeneralized seizures (全身發(fā)作）Mephenytoin 美芬妥英, Ethotoin 乙苯妥英： analogues of phenytoinIneffective for petit mal (absence seizures)Other anticovulsant dru